1. Magnesium-Catalyzed N2-Regioselective Alkylation of 3-Substituted Pyrazoles
- Author
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David H. Russell, Di Xu, Lena Frank, Francis Gosselin, Tina Nguyen, Andreas Stumpf, and Remy Angelaud
- Subjects
010405 organic chemistry ,Magnesium ,Organic Chemistry ,Regioselectivity ,chemistry.chemical_element ,Pyrazole ,Alkylation ,010402 general chemistry ,01 natural sciences ,0104 chemical sciences ,Catalysis ,chemistry.chemical_compound ,chemistry ,Structural isomer ,Organic chemistry - Abstract
A highly regioselective Mg-catalyzed alkylation of 3-substituted pyrazoles has been developed to provide N2-alkylated regioisomers. Using α-bromoacetates and acetamides as alkylating agents, this new method was applied to a variety of 3-substituted and 3,4-disubstituted pyrazoles to produce the N2-alkylated products with high regioselectivities ranging from 76:24 to 99:1 and 44–90% yields.
- Published
- 2019
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